Anti Parkinson Drugs Flashcards
Anti cholinergic drugs bykhlasu keln b —– ma 3ada——
Hydrochloride
Mesylate
Agents that increase dopamine synthesis:
Levodopa:
Transported — to CNs
Converted to dopamine in —-
Only —-% of L dopa reaches the brain
Actively
Brain
1-3
Side effects of levodopa:
1-
2-
3-
4-
1-GI irritation and stimulation of CTZ
2-Upset stomach with nausea and vomiting
3-dyskinesia (involuntary movements)(overactivity of dopamine receptors)
4-mood changes,depression and psychosis
Agents that increase dopamine synthesis:
Dopamine:
Lower doses—-
High doses——
D1 and D2 in——
Effect of binding to D1 nad D2:
Dopamine is metabolized to —– by MAO or COMT
Vasoconstriction on alpha
Stimulates B1 cardiac receptors
Perioheral mesenteric and renal
Vasodlation
Homoooosexua(azde homovanillic acid)
How to increase levodopa in brain?
By carbidopa
Its a decarboxylase inhibitor that prevents metabolization of dopamine in the periphery so more levodopa will reach the brain (10%) and decrease the required levodopa by 5 times
T or F
Carbidopa cross the BBB
Falseee zaddy
Acts peripherally
T or F
Pyridoxine (B6) decrease the breakdown of levodopa in the oeriohery
Ghalaaaaaat
Bl aakesss
Byshtghl b 3aks l bestie carbidopa
T or f
Administration of MAO inhibitors with levodopa can lead to hypertensive crisis
Ehhhhh wley
Agents that inhibit dopamine metabolism
MAO inhibitors
1-
2-
Reversible or rrieversible inhibition?
Khaletna giline
Selegiline
Rasagiline 2nd generation
Irrreeeeeeversible
T or F
COMt trasforms normetadrenaline to VMA
And MAO converts noradrenaline to normetadrenaline
Falseeee
Reverseddd
Khaletna giline is —— administered and —- metabolized
Selegiline bser —– then will lead to —- and ——-
Rasagiline bser ——
Orally
Extensively
Amphetamine
Insomnia and vasoconstriction
1-aminoindan ma eendu vasoactive effect
T or F
Rasagilineee is selective for MAO type A
False
Type B
Agents that inhibit dopamine metabolism
COMT inhibitors
Khaletna —–
Whde m—–w whde m—-
Reversible or itreversible?
Caponeeeee
Whde Tolcapone w whde entacapone
Reversible
COMt transform dopamine to —–
Thus inhibiting it will —-
3 O methyl dopa
Prolong its effect
Inhibition of dopamine metabolism by carbidopa will lead to its metabolism by COMT to ——
This molecule will consequentially —— with —— thus—-
So entacapone is administered to ——
3 o methyl dopa
Compete with levodopa on the active tranport sites
Thus diminish its activity
Reduce methyl o dopa plasma levels by inhibiting COMt